不对称的,立体控制的对甲基胺A的总合成
Robert M Williams1, Jianhua Cao, Hidekazu Tsujishima
1Department of Chemistry, Colorado State University, Fort Collins, Colorado 80523, USA. rmw@chem.colostate.edu
Journal of the American Chemical Society
|October 2, 2003
概括
实现了第一个对甲胺甲的全合成,为这种强大的杀虫剂提供了一条新的途径. 这一突破有效地打击了耐药性肠道寄生虫.
科学领域:
- 有机化学 有机化学
- 药用化学 医学化学
- 药物发现 药物发现 药物发现
背景情况:
- 帕赫尔奎米德A是一种强效的甲虫剂.
- 它显示出对抗耐药性肠道寄生虫的有前途的活动.
- 隔离是来自各种Penicillium物种的.
研究的目的:
- 报告第一个对帕赫奎米德A的总合成.
- 开发一个不对称的,立体控制的合成路线.
- 提供一种有价值的药物化合物的获取.
主要方法:
- 阿尔法-基化-β-基胺衍生物的酶选择性合成.
- 替代的原核的立体控制构造.
- 灾难性选择性分子内S(N) 2'循环对于双循环[2.2.2]diazaoctane核心的形成.
主要成果:
- 顺利完成了第一个对甲基帕赫尔奎米德A的全合成.
- 有效地获得关键的普罗林衍生物.
- 构建复杂的双环[2.2.2]二氧化八环系统,具有较高的二氧化选择性.
结论:
- 报告的合成提供了一个可行的途径,以帕赫奎米德A.
- 这项工作使其治疗潜力的进一步研究成为可能.
- 合成方法可以应用于相关的天然产品.
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